Page last updated: 2024-12-04

apraclonidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

apraclonidine: relieves postoperative intraocular pressure following trabeculoplasty; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

apraclonidine : An imidazoline that is 2-amino 4,5-dihydro-1H-imidazoline in which one of the exocyclic amino hydrogens has been replaced by a 4-amino-2,6-dichlorophenyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2216
CHEMBL ID647
CHEBI ID2788
SCHEMBL ID34127
MeSH IDM0067410

Synonyms (74)

Synonym
AC-12697
PDSP1_000790
PDSP2_000778
NCGC00015033-01
lopac-a-0779
SMP1_000016
D07461
apraclonidine (inn)
LOPAC0_000033
C07668
apraclonidine
66711-21-5
DB00964
4-aminoclonidine
iopidine (tn)
apraclonidinum [inn-latin]
apraclonidine [inn:ban]
apraclonidina [inn-spanish]
2-(4-amino-2,6-dichloro)phenyliminoimidazolidine
1,4-benzenediamine, 2,6-dichloro-n'-(4,5-dihydro-1h-imidazol-2-yl)-
para-aminoclonidine
NCGC00162050-01
L013394
CHEBI:2788 ,
2,6-dichloro-n(1)-(4,5-dihydro-1h-imidazol-2-yl)benzene-1,4-diamine
apraclonidina
apraclonidinum
NCGC00015033-03
CHEMBL647 ,
L000686
2,6-dichloro-1-n-(4,5-dihydro-1h-imidazol-2-yl)benzene-1,4-diamine
2,6-dichloro-n-imidazolidin-2-ylidene-benzene-1,4-diamine(p-aminoclonidine)
p-aminoclonidine2,6-dichloro-n-imidazolidin-2-ylidene-benzene-1,4-diamine
2,6-dichloro-n-imidazolidin-2-ylidene-benzene-1,4-diamine (p-aminoclonidine)
2,6-dichloro-n-imidazolidin-2-ylidene-benzene-1,4-diamine
bdbm50021812
aminoclonidine, p
nsc_51763
bdbm81926
cas_66711-21-5
CCG-204129
NCGC00015033-02
843cen85di ,
unii-843cen85di
aplonidine
FT-0602879
apraclonidine [who-dd]
apraclonidine [mi]
apraclonidine [vandf]
apraclonidine [inn]
gtpl7117
SCHEMBL34127
2,6-dichloro-n1-(4,5-dihydro-1h-imidazol-2-yl)benzene-1,4-diamine
2-(4-amino-2,6-dichlorophenylimino)imidazolidine
2-(4-amino-2,6-dichlorophenylimino) imidazolidine
p-amino clonidine
DTXSID1048415 ,
1,4-benzenediamine, 2,6-dichloro-n1-(4,5-dihydro-1h-imidazol-2-yl)-
2-(4-amino-2,6-dichlorophenylamino)-2-imidazoline
AKOS025401361
HY-12720
Q4781812
2,6-dichloro-n1-(imidazolidin-2-ylidene)benzene-1,4-diamine
SDCCGSBI-0050022.P002
NCGC00015033-04
apraclonidine; lopidine; nc 14; p-aminoclonidine
STARBLD0003083
A918277
CS-0012296
EN300-320403
apraclonidina (inn-spanish)
s01ea03
dtxcid9028388
apraclonidinum (inn-latin)

Research Excerpts

Overview

Apraclonidine hydrochloride is a topical ophthalmic solution with selective alpha-2 and weak alpha-1 receptor agonist activity. It causes Muller muscles to contract quickly elevating the upper eyelid 1-3 mm.

ExcerptReferenceRelevance
"Apraclonidine hydrochloride is a topical ophthalmic solution with selective alpha-2 and weak alpha-1 receptor agonist activity that has the ability to elevate the eye lid."( Apraclonidine in the treatment of ptosis.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
2.62
"Apraclonidine is an alpha-2 adrenergic receptor agonist, which causes contraction of superior tarsal (Müller) muscle which may improve blepharospasm-related eyelid closure."( Treatment of blepharospasm with apraclonidine.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
1.46
"Apraclonidine is a potentially useful medication for short term management of blepharospasm symptoms while awaiting botulinum toxin injection."( Treatment of blepharospasm with apraclonidine.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
2.18
"Apraclonidine seems to be a good alternative to cocaine to confirm Horner's syndrome."( [Acquired Horner's syndrome].
Alstadhaug, KB, 2011
)
1.09
"Apraclonidine is an alpha2-adrenergic agonist, which causes Muller muscles to contract quickly elevating the upper eyelid 1-3 mm."( The use of apraclonidine eyedrops to treat ptosis after the administration of botulinum toxin to the upper face.
Scheinfeld, N, 2005
)
1.44
"Apraclonidine eye drop is an alpha adrenergic agonist derived topical clonidine, used for the treatment of intraocular pressure elevation. "( More than just an ocular solution.
Karakus, G; Pekdemir, M; Yanturali, S, 2005
)
1.77
"Apraclonidine is a safe and readily available alternative to cocaine for the diagnosis of Horner syndrome."( Effect of 0.5% apraclonidine on ptosis in Horner syndrome.
Garibaldi, DC; Grant, MP; Hindman, HB; Iliff, NT; Merbs, SL,
)
1.21
"Apraclonidine is a alpha 2 adrenergic agonic which is a para-amino derivative of clonidine. "( [Effect and side effects of apraclonidine].
Stewart, WC, 1996
)
2.03
"Apraclonidine hydrochloride is a derivative of clonidine hydrochloride, an alpha 2-adrenergic agonist."( New developments in the drug treatment of glaucoma.
Crawford, K; Hurvitz, LM; Kaufman, PL; Robin, AL; Shaw, B; Weinreb, RN, 1991
)
1

Effects

Apraclonidine 1.0% has been shown to reverse the potential intraocular pressure (IOP) increase after pupil dilation in patients with chronic open-angle glaucoma.

ExcerptReferenceRelevance
"Apraclonidine has been used as a diagnostic test in Horner's syndrome."( Apraclonidine in the treatment of ptosis.
Jankovic, J; Vijayakumar, D; Wijemanne, S, 2017
)
2.62
"Apraclonidine eye drops have been suggested to diagnose Horner syndrome."( The pupil.
Wilhelm, H, 2008
)
1.07
"Apraclonidine 1.0% has been shown to reverse the potential intraocular pressure (IOP) increase after pupil dilation IOP increases in patients with chronic open-angle glaucoma. "( Reversal of intraocular pressure increases with 0.5% apraclonidine after dilated fundus examination in patients with chronic open-angle glaucoma.
Chang, FW; Kolin, T; Nishimoto, JH; Tang, IH, 1999
)
2

Actions

ExcerptReferenceRelevance
"Apraclonidine 0.5% did not produce a significant effect on pupil diameter."( Pupillometry study of brimonidine tartrate 0.2% and apraclonidine 0.5%.
Besada, E; Hardigan, P; Najman, P; Reed, K; Shechtman, D, 2011
)
1.34

Treatment

Apraclonidine treatment resulted in significantly more patients attaining an additional 20% reduction or more in intraocular pressure from baseline. The IOP fell from a mean of 15.6 +/- 3.8 to 12.8 +/- 6.0 mm Hg three hours postoperatively.

ExcerptReferenceRelevance
"Apraclonidine treatment resulted in significantly more patients attaining an additional 20% reduction or more in intraocular pressure from baseline and an intraocular pressure less than or equal to 20 mm Hg (P < .05)."( Short-term efficacy of apraclonidine hydrochloride added to maximum-tolerated medical therapy for glaucoma. Apraclonidine Maximum-Tolerated Medical Therapy Study Group.
Lehmann, RP; Mundorf, T; Ritch, R; Robin, AL; Shin, DH; Smythe, B, 1995
)
1.32
"Apraclonidine-treated eyes showed mydriasis and blanching of the conjunctiva."( Apraclonidine protection of the blood-aqueous barrier from traumatic break-down.
Bellucci, R; Bonomi, L; Pagliarusco, A; Stefani, L, 1995
)
2.46
"Apraclonidine treatment resulted in significantly more patients achieving either an additional > or = 20% reduction in IOP from baseline (resulting in an IOP < or = 20 mm Hg) (P < 0.05)."( Topical apraclonidine hydrochloride in eyes with poorly controlled glaucoma. The Apraclonidine Maximum Tolerated Medical Therapy Study Group.
Lehmann, RP; Mundorf, T; Ritch, R; Robin, AL; Shin, D; Smythe, B, 1995
)
1.45
"In apraclonidine-treated eyes the IOP fell from a mean of 15.6 +/- 3.8 mm Hg to 12.8 +/- 6.0 mm Hg 3 hours postoperatively (P less than .001)."( Effectiveness of apraclonidine in preventing the rise in intraocular pressure after neodymium:YAG posterior capsulotomy.
Brown, RH; Crandall, AS; Pollack, IP; Robin, AL; Stewart, RH; White, GL, 1988
)
1.13
"In apraclonidine-treated eyes, the IOP fell from a mean of 15.6 +/- 3.8 to 12.8 +/- 6.0 mm Hg three hours postoperatively."( Prevention of the rise in intraocular pressure following neodymium-YAG posterior capsulotomy using topical 1% apraclonidine.
Brown, RH; Crandall, AS; Pollack, IP; Robin, AL; Stewart, RH; White, GL, 1988
)
1

Toxicity

Apraclonidine is well tolerated systemically with no serious adverse event attributed previously to this medicine. We report adverse effects when used in the diagnosis of Horner syndrome in infants.

ExcerptReferenceRelevance
" Apraclonidine is well tolerated systemically with no serious adverse event attributed previously to this medicine."( [Effect and side effects of apraclonidine].
Stewart, WC, 1996
)
1.5
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"(3,4) We report adverse effects of topical apraclonidine when used in the diagnosis of Horner syndrome in infants."( Adverse effects of apraclonidine used in the diagnosis of Horner syndrome in infants.
Lim, MK; Satterfield, D; Watts, P, 2007
)
0.93

Bioavailability

ExcerptReferenceRelevance
" To understand the implications for retina-optic nerve vascular physiology and pathophysiology, studies of the exact location of the binding sites, the bioavailability of the adrenergic agonists, and the physiological responses to receptor stimulation in both normal and pathological states are required."( Adrenergic alpha 1 and alpha 2 binding sites are present in bovine retinal blood vessels.
Anderson, DR; Ferrari-Dileo, G; Forster, BA, 1987
)
0.27
" Addition of clonidine to the formulations decreased the systemic absorption rate of the anesthetics from the patch application site without impacting the coating performance or the rapid onset of anesthesia."( Adjuvants to prolong the local anesthetic effects of coated microneedle products.
Brown, K; Dohmeier, D; Hansen, K; Siebenaler, K; Zhang, Y, 2012
)
0.38

Dosage Studied

We performed a double-masked, cross-over, dose-response study of apraclonidine hydrochloride (formerly known as ALO 2145) in 20 patients with elevated intraocular pressure (IOP)

ExcerptRelevanceReference
" ALO 2145 1% was shown to be effective and well tolerated in the dosage regimen employed in this study."( [Efficacy and tolerability of apraclonidine (ALO 2145, 1%) in the prevention of early ocular hypertonia, after trabeculoretraction using argon laser and posterior capsulotomy using Nd:YAG laser].
Berrod, JP; Raspiller, A, 1992
)
0.57
" IAP pretreatment also caused a marked upward shift in the dose-response curve of vasopressin (10(-10) to 10(-4) M)-induced cAMP accumulation."( Tonic inhibition of renal response to vasopressin by a pertussis toxin substrate.
Fallet, R; Gong, GD; Jeffries, WB; Pettinger, WA; Van Dreal, P, 1988
)
0.27
"We performed a double-masked, cross-over, dose-response study of apraclonidine hydrochloride (formerly known as ALO 2145) in 20 patients with elevated intraocular pressure (IOP)."( Apraclonidine. A one-week dose-response study.
Jampel, HD; Pollack, IP; Quigley, HA; Robin, AL, 1988
)
1.96
" Dose-response curves were generated for para-aminoclonidine in the presence of vehicle alone, yohimbine (alpha-2 antagonist), idazoxan (alpha-2/I1/I2 antagonist) and prazosin (alpha-1 antagonist)."( Identification, localization and functional analysis of imidazoline and alpha adrenergic receptors in canine prostate.
Breslin, DS; Ernsberger, P; Felsen, D; Marion, DN; May, M; Nejat, RJ; Nguyen, P; Sutaria, PM; Vaughan, ED, 1994
)
0.29
"5% timolol maleate twice daily for at least 4 weeks and who had 8 AM IOPs of at least 22 mm Hg and no greater than 30 mm Hg 12 hours after dosing were eligible for the study."( The efficacy of apraclonidine as an adjunct to timolol therapy. Apraclonidine Adjunctive Therapy Study Group.
Lehmann, RP; Ritch, R; Shin, DH; Shrader, CE; Stewart, WC; van Buskirk, EM, 1995
)
0.64
"5% timolol 8 hours after dosing on days 1, 30, and 90; and a significant difference (P < ."( A 90-day study of the efficacy and side effects of 0.25% and 0.5% apraclonidine vs 0.5% timolol. Apraclonidine Primary Therapy Study Group.
Horwitz, B; Kottler, M; Laibovitz, R; Ritch, R; Stewart, RH; Stewart, WC, 1996
)
0.53
" The effects of two different dosage regimens, once before surgery or once before and after surgery, were studied."( The effect of 1% apraclonidine on intraocular pressure after cataract surgery.
Renzenbrink-Bubberman, AC; Sterk, CC; van Best, JA, 1998
)
0.64
" Research needs to be done to establish the utility and dosing of apraclonidine for botulinum toxin-induced ptosis."( The use of apraclonidine eyedrops to treat ptosis after the administration of botulinum toxin to the upper face.
Scheinfeld, N, 2005
)
0.96
"Each of the single topical drugs produced significant dose-dependent antiallodynic effects compared with vehicle in CPIP rats (N = 30), and the antiallodynic dose-response curves of either PA or PDE inhibitors were shifted 5- to 10-fold to the left when combined with nonanalgesic doses of α2A receptor agonists or NO donors (N = 28)."( Topical combinations to treat microvascular dysfunction of chronic postischemia pain.
Abaji, R; Coderre, TJ; Laferrière, A; Ragavendran, JV; Tsai, CY, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
alpha-adrenergic agonistAn agent that selectively binds to and activates alpha-adrenergic receptors.
antiglaucoma drugAny drug which can be used to prevent or alleviate glaucoma, a disease in which the optic nerve is damaged, resulting in progressive, irreversible loss of vision. It is often, though not always, associated with increased pressure of the fluid in the eye.
ophthalmology drugAny compound used for the treatment of eye conditions or eye diseases.
beta-adrenergic agonistAn agent that selectively binds to and activates beta-adrenergic receptors.
diagnostic agentA substance administered to aid diagnosis of a disease.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
imidazolinesDiazoline compounds having the nitrogen atoms at the 1- and 3-positions and a double bond at an unspecified position.
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency1.25890.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency1.25890.025120.237639.8107AID886
NFKB1 protein, partialHomo sapiens (human)Potency28.18380.02827.055915.8489AID895; AID928
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency16.81760.531815.435837.6858AID504845
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency28.18380.00106.000935.4813AID943
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.60120.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00400.00001.44217.3470AID36188
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.00290.00010.807410.0000AID35946
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00400.00001.23808.1590AID36188
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00400.00001.47257.8980AID36188
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.03000.00030.483410.0000AID36404
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00480.00000.929610.0000AID36373
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.18000.00000.360910.0000AID36104
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.18000.00000.272610.0000AID36104
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.18000.00000.471310.0000AID36104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00190.00080.37336.7100AID36512
Alpha-2B adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00190.00051.36446.7100AID36512
Alpha-2C adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00190.00050.55416.7100AID36512
Alpha-1D adrenergic receptorHomo sapiens (human)EC50 (µMol)0.18000.00151.72275.6000AID36261
Adenosine receptor A2bRattus norvegicus (Norway rat)EC50 (µMol)0.00190.00190.19330.7200AID36512
Adenosine receptor A2aRattus norvegicus (Norway rat)EC50 (µMol)0.00190.00000.11560.7200AID36512
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.18000.00010.50987.1000AID36261
Alpha-1B adrenergic receptorHomo sapiens (human)EC50 (µMol)0.18000.00011.30105.6000AID36261
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (80)

Processvia Protein(s)Taxonomy
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID36261Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID36404Compound was tested in vitro for binding affinity against Alpha-2C adrenergic receptor from cloned human C-2 receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID36188Inhibition of [3H]p-aminoclonidine (PAC) binding to alpha-2 adrenergic receptor of purified human platelet plasma membranes1987Journal of medicinal chemistry, Jul, Volume: 30, Issue:7
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID36104Compound was tested for binding affinity based on dissociation constant of Alpha-1 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID177376In vivo ED40 is the raising diastolic blood pressure by 40 mm Hg in pithed rats. (postjunctional)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID173991In vivo dose required to inhibit vas deferens contraction by 25% after pretreatment with prazosin in pithed rats. (prejunctional)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Indoline analogues of idazoxan: potent alpha 2-antagonists and alpha 1-agonists.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID36512Compound was tested for concentration that produced 50% contractile relative response to maximum response to norepinephrine for Alpha-2 adrenergic receptor1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID35946Compound was tested in vitro for binding affinity against Alpha-2A adrenergic receptor from cloned human C-10 receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID36373Compound was tested in vitro for binding affinity against Alpha-2B adrenergic receptor from cloned rat RNG receptor transfected into Chinese hamster ovary (CHO) cells1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID36661Inhibitory activity against Alpha-2 adrenergic receptor in rat vas deferens1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Heteroaromatic analogues of the alpha 2-adrenoreceptor partial agonist clonidine.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1996Journal of medicinal chemistry, Aug-30, Volume: 39, Issue:18
Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (400)

TimeframeStudies, This Drug (%)All Drugs %
pre-199098 (24.50)18.7374
1990's169 (42.25)18.2507
2000's72 (18.00)29.6817
2010's47 (11.75)24.3611
2020's14 (3.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.01

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index57.01 (24.57)
Research Supply Index6.27 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index123.00 (26.88)
Search Engine Supply Index2.56 (0.95)

This Compound (57.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials98 (22.95%)5.53%
Reviews24 (5.62%)6.00%
Case Studies52 (12.18%)4.05%
Observational1 (0.23%)0.25%
Other252 (59.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficacy of Apraclonidine Eye Drops in the Treatment of Ptosis Secondary to Myasthenia Gravis [NCT05045248]Phase 210 participants (Actual)Interventional2020-06-01Completed
Comparison of the Alpha-2 Agonists for Prevention of Intraocular Pressure Elevation After Selective Laser Trabeculoplasty [NCT00567411]43 participants (Anticipated)Interventional2006-08-31Recruiting
Efficacy of Topical Apraclonidine for the Treatment of Ocular Synkinesis [NCT05167760]Phase 410 participants (Anticipated)Interventional2023-12-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]